Z-ligustilide: A review of its pharmacokinetics and pharmacology

Phytother Res. 2020 Aug;34(8):1966-1991. doi: 10.1002/ptr.6662. Epub 2020 Mar 5.


Z-ligustilide is a natural benzoquinone derivative found in many widely used Chinese herbal medicines such as Angelica sinensis (Oliv.) Diels as well as Ligusticum chuanxiong Hort and so on. It has been used as a part of traditional Chinese medicine and is also present in various Chinese medicine preparations. Pharmacokinetic studies have shown that Z-ligustilide has poor oral bioavailability in rats due to severe first-pass metabolic reactions. New evidence suggests that Z-ligustilide has a wide range of pharmacological properties, including anticancer, antiinflammatory, anti-oxidant as well as neuroprotective activities and so on. The literature discussed is derived from readily accessible papers spanning the early 1970s to the end of March 2019. Information were collected from journals, books, and online searches (Google Scholar, PubMed, Science Direct, Science Citation Index Finder, Springer link, and CNKI). This review intends to provide a comprehensive overview of the pharmacokinetics and pharmacology of Z-ligustilide in recent years, with a focus on its biological properties and mechanisms, which is of great significance for Chinese medicine.

Keywords: Z-ligustilide; mechanisms; pharmacokinetics; pharmacology.

Publication types

  • Review

MeSH terms

  • 4-Butyrolactone / analogs & derivatives*
  • 4-Butyrolactone / pharmacokinetics
  • 4-Butyrolactone / pharmacology
  • 4-Butyrolactone / therapeutic use
  • Animals
  • Drugs, Chinese Herbal / pharmacokinetics
  • Drugs, Chinese Herbal / pharmacology
  • Drugs, Chinese Herbal / therapeutic use*
  • Humans
  • Molecular Structure
  • Rats


  • Drugs, Chinese Herbal
  • ligustilide
  • 4-Butyrolactone